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Aim:To investigate the modulatory effect of CJZ3,a lomerizine derivative,on P-glycoprotein (P-gp) function in rat brain microvessel endothelial cells (RBMEC).Methods:RBMEC were isolated and cultured in Dulbecco’s modified Eagle’s medium/F12 (1∶1) medium,and the amount of intracellular rhodamine 123 (Rh123) was determined using a fluorescence spectrophotometer to evaluate the modulatory effect of CJZ3 on P-gp function.Results:The accumulation of Rh123 was 190ten. tiated in a concentration-dependent manner after incubation witll CJZ3 for RBMEC.but not for human umbilical vein endothelial cells (HUVEC).CJZ3 caused the accumulation of intracellular Rh 123 in a time.dependent manner and significantly decreased the effiUX of Rhl 23 from the cells.The inhibitory effect of CJZ3 on P-gp function was reversible and remained for 120 min after CJZ3 (2.5 μmol/L) was removed from the medium.Conclusion:CJZ3 has a potent in vitro effect on the inhibition of P-gp function.